新型抗癌药依托泊苷脂质体的制备

郑宁;张立德

中国药学杂志 ›› 2004, Vol. 39 ›› Issue (03) : 202-204.

中国药学杂志 ›› 2004, Vol. 39 ›› Issue (03) : 202-204.
论著

新型抗癌药依托泊苷脂质体的制备

  • 郑宁;张立德
作者信息 +

Preparation of a new antitumor drug etoposide-loaded liposomes

  • ZHENG Ning1;ZHANG Li-de2
Author information +
文章历史 +

摘要

目的 制备依托泊苷脂质体,测定其含药量及包封率,对其体外释放及原料药的体外释放进行比较,并对脂质体灭菌后的稳定性进行考察。方法 采用薄膜-超声分散法制备依托泊苷脂质体,通过均匀设计优化处方,利用透析法测定其含药量及包封率,进行热压灭菌及60Co灭菌两种灭菌方式,以粒径和包封率为指标考证灭菌后的稳定性。结果 按均匀设计的最优组合制备脂质体的含药量为(574.3±30.7)μg·mL-1,平均包封率为(61.58±0.83)%,依托泊苷脂质体50 h累积释药(96.13±1.11)%,而其原料药3 h累积释药(97.10±1.84)%,热压灭菌的渗漏率比60Co灭菌的渗漏率高。结论 用薄膜-超声分散法制备的依托泊苷脂质体外观圆整,粒径小而均匀,体外释药达到了长效缓释的作用,60Co灭菌后脂质体较稳定。

Abstract

OBJECTIVE To prepare etoposide-loaded liposomes, determine its drug content and encapsulation efficiency, compare its in vitro release with that of etoposide power,and study its stability after sterilization METHODS The etoposide-loaded liposomes were prepared by film- ultrasonic wave dissolving techniques. The optimum formula was selected through uniform design. Dialytic method was used to determine drug content and encapsulation efficiency. Moist heat sterlization and60 Co radiation sterilization were applied. The vesicle size and percolation rate were used as stability parameters RESULTS The drug content of etoposide-loaded liposomes prepared by the optimum formular was (574.3±30.7)μg·mL-1. The average encapsulation efficiency was (61.58±0.83)%. The in vitro release of etoposide-loaded liposomes added up to (96.13±1.11)% in 50 h. The release of etoposide powder added up to (97.10±1.84)% in 3 h.The average percolation rate was higher with moist heat sterilization than with sterilization by60 Co radiation CONCLUSION The etoposide-loaded liposomes prepared by film- ultrasonic wave dissolving techniques were regular in morphology, and their vesicle sizes were small and even. The liposomes were conformed to be sustained-release preparation through in vitro release experiments. They were stable after60 Co radiation sterilization.

关键词

依托泊普 / 脂质体

Key words

etoposide / liposomes / sterilization

引用本文

导出引用
郑宁;张立德. 新型抗癌药依托泊苷脂质体的制备[J]. 中国药学杂志, 2004, 39(03): 202-204
ZHENG Ning;ZHNG Li-de. Preparation of a new antitumor drug etoposide-loaded liposomes[J]. Chinese Pharmaceutical Journal, 2004, 39(03): 202-204

参考文献

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